AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPsychiatry and PsychologyPhenomena and Processes
Cannabinoid Receptor AgonistsReceptors, CannabinoidCannabinolCannabinoidsReceptor, Cannabinoid, CB1Receptor, Cannabinoid, CB2BenzoxazinesCyclohexanolsNaphthalenesCannabinoid Receptor AntagonistsDronabinolCannabinoid Receptor ModulatorsReceptors, DrugMorpholinesEndocannabinoidsPyrazolesPolyunsaturated AlkamidesPiperidinesBornanesArachidonic AcidsAnalgesicsGlyceridesDose-Response Relationship, DrugAmidohydrolasesRats, Sprague-DawleyCannabidiolPainDrug InteractionsImmunologic FactorsCalcium Channel BlockersRats, WistarMonoacylglycerol LipasesMice, Inbred C57BLSynaptic TransmissionPurinergic P1 Receptor AgonistsSignal TransductionCells, CulturedPain MeasurementSerotonin Receptor AgonistsNeuronsDopamine AgonistsDisease Models, AnimalCannabisSerotonin 5-HT1 Receptor AgonistsSerotonin 5-HT2 Receptor AgonistsAdenosine A1 Receptor AgonistsLigandsImmunomodulationIndolesMice, KnockoutReceptors, Opioid, muRadioligand AssayGuanosine 5'-O-(3-Thiotriphosphate)GABA AgonistsReceptors, Opioid, kappaAdenosine A2 Receptor AgonistsCHO CellsGABA-A Receptor AgonistsBehavior, AnimalGABA-B Receptor AgonistsSerotonin 5-HT4 Receptor AgonistsBrainDrug Inverse AgonismCricetinaeAdrenergic alpha-2 Receptor AgonistsPurinergic P2 Receptor AgonistsHippocampusCarbamatesEthanolaminesCyclic AMPEnkephalin, Ala(2)-MePhe(4)-Gly(5)-TRPV Cation ChannelsReceptors, OpioidRNA, MessengerCell LineBenzodioxolesBinding, CompetitiveReceptors, Dopamine D2CapsaicinResorcinolsMice, Inbred ICRPertussis ToxinTime Factorsgamma-Aminobutyric AcidReceptors, G-Protein-CoupledAdenosine A3 Receptor AgonistsExcitatory Amino Acid AgonistsCytokinesMuscarinic AgonistsHallucinogensHistamine AgonistsAdenosineMotor ActivityAdjuvants, ImmunologicDrug ToleranceCalciumPatch-Clamp TechniquesHyperalgesiaCyclohexanes
Endocannabinoid SystemEndogenousCannabisTherapeuticPeripheralPsychoactiveProtein-coupledSyntheticVitroTetrahydrocannabinolAntagonistCompoundsOrallyEC50AffinityStructurallyModulatorBindsLigand-activatedEvidenceHypersensitivityInhibitsSelectiveEffectsImmuneTypeAcidResistanceMolecularActivationFoundBrainTreatmentStudyClassChemical
Endocannabinoid System1
  • Its identification proved that the endocannabinoid system was responsible for more than just mediating the effects of plant-based cannabinoids like THC. (effectivenewsletter.com)
Endogenous4
Cannabis8
  • The objective of this study was to evaluate the anti-inflammatory properties of selected cannabis-derived terpenes and cannabinoids. (bvsalud.org)
  • Overall, these studies suggest that selected cannabis-derived terpenes displayed minimal immunological activity, while cannabinoids exhibited a broader range of activity. (bvsalud.org)
  • A Cannabis product that contains all of the original compounds found in Cannabis flower - cannabinoids, terpenes, and flavonoids - and from which tetrahydrocannabinol (THC) has been removed. (effectivenewsletter.com)
  • Cannabinoids ( / k ə ˈ n æ b ə n ɔɪ d z ˌ ˈ k æ n ə b ə n ɔɪ d z / ) are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. (cloudfront.net)
  • [1] [2] The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary psychoactive compound in cannabis . (cloudfront.net)
  • At least 113 different cannabinoids have been isolated from the Cannabis plant. (cloudfront.net)
  • These cannabinoids produce the effects associated with cannabis by binding to the CB 1 cannabinoid receptors in the brain. (cloudfront.net)
  • This manuscript in-depth review will investigate the potential of the ECS in the treatment of various diseases, and to put forth the suggestion that many of these secondary metabolites of Cannabis sativa L. (hereafter referred to as " C. sativa L." or "medical cannabis"), may also have potential as lead compounds in the development of cannabinoid-based pharmaceuticals for a variety of diseases. (thctotalhealthcare.com)
Therapeutic4
  • In this review article, we will focus on a broad range of cannabinoids, their receptor dependent and receptor independent functional roles against various cancer types with respect to growth, metastasis, energy metabolism, immune environment, stemness and future perspectives in exploring new possible therapeutic opportunities. (oncotarget.com)
  • Arevalo-Martin A, Vela JM, Molina-Holgado E, Borrell J, Guaza C. Therapeutic action of cannabinoids in a murine model of multiple sclerosis. (cialisonlinecialispricehnn.com)
  • [20] CB 2 receptors appear to be responsible for immunomodulatory [19] and possibly other therapeutic effects of cannabinoid as seen in vitro and in animal models. (cloudfront.net)
  • The distribution of the components of the ECS system throughout the body, and the physiological/pathophysiological role of the ECS-signalling pathways in many diseases, all offer promising opportunities for the development of novel cannabinergic, cannabimimetic, and cannabinoid-based therapeutic drugs that genetically or pharmacologically modulate the ECS via inhibition of metabolic pathways and/or agonism or antagonism of the receptors of the ECS. (thctotalhealthcare.com)
Peripheral4
  • Identification of in vitro metabolites of JWH-015, an aminoalkylindole agonist for the peripheral cannabinoid receptor (CB2) by HPLC-MS/MS". Analytical and Bioanalytical Chemistry. (wikipedia.org)
  • Cannabinoid is a family of complex chemicals (terpenophenolic compounds) that exert most of their actions by binding to and activating specific Gαi protein-coupled receptors named as cannabinoid receptor, CB1 (Central receptor) and CB2 (Peripheral receptor) respectively [ 4 - 5 ]. (oncotarget.com)
  • Ozanimod, sold under the brand name Zeposia, is an immunomodulatory medication for the treatment of relapsing multiple sclerosis (RMS) and ulcerative colitis.It acts as a sphingosine-1-phosphate (S1P) receptor agonist, sequestering lymphocytes to peripheral lymphoid organs and away from their sites of chronic inflammation. (csnpharm.cn)
  • KRP-203 is a selective Sphingosine-1-phosphate receptor agonist that has been shown to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models. (csnpharm.cn)
Psychoactive2
  • JWH-018 is a potent synthetic cannabinoid agonist that has been shown to produce powerful psychoactive effects in humans. (deltabioresearchchemicals.com)
  • CB1 receptors are ubiquitously located, with their highest presence found in the central nervous system (basal ganglia, hippocampus, cerebellum and cortex) where they mediate cannabinoid psychoactive effects [ 7 - 8 ]. (oncotarget.com)
Protein-coupled1
  • [12] The human brain has more cannabinoid receptors than any other G protein-coupled receptor (GPCR) type. (cloudfront.net)
Synthetic3
Vitro2
  • JWH-015 has been shown in vitro to be metabolized primarily by hydroxylation and N-dealkylation, and also by epoxidation of the naphthalene ring, similar to the metabolic pathways seen for other aminoalkylindole cannabinoids such as WIN 55,212-2. (wikipedia.org)
  • In vitro, JWH-015 has been shown to be a more potent agonist of the CB2 receptor than THC, with an EC50 value of 0.37 nM compared to 1.43 nM for THC. (deltabioresearchchemicals.com)
Tetrahydrocannabinol2
Antagonist6
  • W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM. (csnpharm.cn)
  • TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor. (csnpharm.cn)
  • ONO-7300243 is a potent LPA1 (Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM. (csnpharm.cn)
  • JTE 013 is a potent, selective S1P2 receptor antagonist with IC50 value of 17.6 nM. (csnpharm.cn)
  • GLPG2938 is a pontent antagonist of S1P2 receptor, with exquisite potency on a phenotypic IL8 release assay, good pharmacokinetics, and good activity in a bleomycin-induced model of pulmonary fibrosis. (csnpharm.cn)
  • CYM50358 is a potent S1PR4 antagonist with an IC50 of 25 nM. (csnpharm.cn)
Compounds1
  • Cannabinoids are the active compounds of this marijuana plant. (oncotarget.com)
Orally1
  • TC-G 1006 is a potent and orally active S1P1 agonist with EC50 of 18 nM, showing no activity on S1P3. (csnpharm.cn)
EC504
  • JWH is a potent agonist at cannabinoid type- (CB) and cannabinoid type- (CB) receptors, with EC50 values of 0.89 nM and 1.43 nM respectively. (deltabioresearchchemicals.com)
  • Siponimod is a selective S1P1 receptor modulator with EC50 of 0.4 nM, approved for treatment for secondary progressive multiple sclerosis. (csnpharm.cn)
  • Activates S1P1 receptor with an EC50 of 13 nM, but does not activate S1P2, S1P3, S1P4 or S1P5 receptors at concentrations up to 10 μM. (csnpharm.cn)
  • Ponesimod is a selective S1P1 receptor modulator with EC50 of 5.7 nM, used in the reserch of treatment of multiple sclerosis (MS) and psoriasis. (csnpharm.cn)
Affinity2
  • Its affinity for CB2 receptors is 13.8 nM, while its affinity for CB1 is 383 nM, meaning that it binds almost 28 times more strongly to CB2 than to CB1. (wikipedia.org)
  • It has been shown to bind to both CB1 and CB2 receptors with high affinity and to produce similar effects to those seen with other cannabinoids such as THC. (deltabioresearchchemicals.com)
Structurally1
  • It can be found in some herbal incense blends and is structurally similar to the naturally occurring cannabinoid THC. (deltabioresearchchemicals.com)
Modulator2
  • Siponimod, sold under the brand name Mayzent, is a selective sphingosine-1-phosphate receptor modulator for oral use that is used for multiple sclerosis (MS). It is intended for once-daily oral administration. (csnpharm.cn)
  • Ozanimod is an oral, once daily, selective sphingosine 1-phosphate 1 and 5 receptor modulator in development for autoimmune indications including relapsing multiple sclerosis (RMS) and ulcerative colitis (UC). (csnpharm.cn)
Binds2
  • A chemical that binds to a receptor and increases its activity. (effectivenewsletter.com)
  • The measure of how well a chemical binds to a receptor, which impacts how strongly the cell associated with the receptor reacts. (effectivenewsletter.com)
Ligand-activated3
  • The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor influencing many biological processes in diverse cell types. (bvsalud.org)
  • Previous studies have demonstrated that activation of the aryl hydrocarbon receptor (AHR), a cytosolic ligand-activated transcription factor, results in suppressed IgM responses and is dependent on LCK. (bvsalud.org)
  • Plants sense abscisic acid (ABA) using chemical-induced dimerization (CID) modules, including the receptor PYR1 and HAB1, a phosphatase inhibited by ligand-activated PYR1. (nature.com)
Evidence2
  • Epoxidation of polycyclic aromatic hydrocarbons (see for example benzo(a)pyrene toxicity) can produce carcinogenic metabolites, although there is no evidence to show that JWH-015 or other aminoalkylindole cannabinoids are actually carcinogenic in vivo. (wikipedia.org)
  • Two known cannabinoid receptors are termed CB 1 and CB 2 , [11] with mounting evidence of more. (cloudfront.net)
Hypersensitivity1
  • RP001 is a sphingosine-1-phosphate receptor 1 agonist which inhibits tertiary lymphoid tissue reactivation and hypersensitivity in the lung. (csnpharm.cn)
Inhibits2
  • A major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). (effectivenewsletter.com)
  • inhibits S1P1 and S1P3 receptors (pKi values are 7.86 and 5.93 respectively). (csnpharm.cn)
Selective6
  • JWH-015 is a chemical from the naphthoylindole family that acts as a subtype-selective cannabinoid agonist. (wikipedia.org)
  • However, it still displays some CB1 activity, and in some model systems can be very potent and efficacious at activating CB1 receptors, and therefore it is not as selective as newer drugs such as JWH-133. (wikipedia.org)
  • SEW2871 is a potent and selective sphingosine-1-phosphate 1 (S1P1) receptor agonist. (csnpharm.cn)
  • It has antioxidant property and inhibites HIV-1 replication in MT-2 cell culture at non-toxic concentrations, a potent and highly selective class of HIV-1 integrase inhibitors. (csnpharm.cn)
  • CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist. (csnpharm.cn)
  • Ceralifimod (ONO-4641) is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively. (csnpharm.cn)
Effects6
  • It has been shown to possess immunomodulatory effects, and CB2 agonists may be useful in the treatment of pain and inflammation. (wikipedia.org)
  • It has been shown to produce antinociceptive, neuroprotective, and immunomodulatory effects in various animal models. (deltabioresearchchemicals.com)
  • The exact mechanisms by which JWH produces these effects are not fully understood, but they are thought to involve activation of both CB1 and CB2 receptors. (deltabioresearchchemicals.com)
  • Though cannabinoids are clinically used for anti-palliative effects, recent studies open a promising possibility as anti-cancer agents. (oncotarget.com)
  • This group means that acid cannabinoids are metabolized in different ways by the body, and don't necessarily cause the same effects as their 'active' counterparts. (effectivenewsletter.com)
  • Before the 1980s, cannabinoids were speculated to produce their physiological and behavioral effects via nonspecific interaction with cell membranes , instead of interacting with specific membrane-bound receptors . (cloudfront.net)
Immune1
  • Of the 21 responses assayed for each compound, cannabinoids showed the greatest immune modulating activity compared to their vehicle control. (bvsalud.org)
Type1
Acid2
  • Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells. (nottingham.ac.uk)
  • Several studies have uncovered potent biological activities of 2-hydroxyoleic acid (Minerval). (gerli.com)
Resistance1
  • ABA is a stress hormone perceived by the soluble receptor PYR1 (encoded by Pyrabactin resistance 1 ) and its related PYR1- like and R egulatory C omponent of ABA R ecepto r proteins ( PYL/RCAR , PYLs for simplicity) 18 . (nature.com)
Molecular1
  • This discovery has opened the way to identification of the molecular action of various cannabinoids and the cannabinoid receptors. (oncotarget.com)
Activation2
  • It was reported that activation of CB1 receptors by locally released anandamide may participate in the control of bronchial contractility. (cialisonlinecialispricehnn.com)
  • Risk factors for depression initiate an infection-like inflammation in the brain that involves activation microglial Toll-like receptors and glycogen synthase kinase-3β (GSK3β). (mdpi.com)
Found1
  • CB 1 receptors are found primarily in the brain , more specifically in the basal ganglia and in the limbic system , including the hippocampus [11] and the striatum . (cloudfront.net)
Brain1
  • CB 1 receptors are absent in the medulla oblongata , the part of the brain stem responsible for respiratory and cardiovascular functions. (cloudfront.net)
Treatment1
  • GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis. (csnpharm.cn)
Study1
Class1
  • In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-015 are Schedule I Controlled Substances. (wikipedia.org)
Chemical1
  • These forms have an extra chemical group, called a carboxyl group, that makes the cannabinoid slightly larger than the more familiar, 'activate', forms (like Δ9-THC and CBD). (effectivenewsletter.com)